FBS-Derived Exosomes as a Natural Nano-Scale Carrier for Icariin Promote Osteoblast Proliferation

Abstract

Icariin is a class IV drug of low solubility, permeability, and poor bioavailability. Synthetic nanomaterials have developed rapidly. However, some literatures point out that synthetic nanomaterials such as liposomes, aptamers, metal nanoparticles, and nanogels have high toxicity and are affected by the reticuloendothelial system or mononuclear phagocyte system. It is known that exosomes could be used as an ideal clinical drug delivery vehicle to avoid the above-mentioned problems to a certain extent. Studies have shown that drugs can be loaded into exosomes by passive and active loading. We used Fetal bovine serum (FBS) exosomes to carry Icariin for the first time in this experiment, FBS exosomes-Icariin (FBS EXO-ICA) more effectively promoted the proliferation of osteoblasts and bone regeneration than Icariin alone. FBS EXO-ICA could become a new nano scale drug formulation for treating diseases associated with bone loss.

Bone Mesenchymal Stem Cell-Derived sEV-Encapsulated Thermosensitive Hydrogels Accelerate Osteogenesis and Angiogenesis by Release of Exosomal miR-21

“…Because of their ideal characteristics, sEVs are also favorable nanoscale drug carriers for the regeneration of tissues and the treatment of certain diseases ( Liao et al, 2019a ; Elsharkasy et al, 2020 ). For example, Dong et al revealed that the use of fetal bovine serum-derived sEVs to carry Icariin could promote osteoblast proliferation and bone regeneration more effectively than Icariin alone ( Dong et al, 2021 ). Wu et al demonstrated that BMSC-derived sEVs and Fe 3 O 4 nanoparticles under conditions of a static magnetic field could facilitate bone regeneration and enhance wound healing ( Wu et al, 2020 ; Wu et al, 2021 ).…”

Icariin attenuates renal fibrosis in chronic kidney disease by inhibiting interleukin‐1β/transforming growth factor‐β‐mediated activation of renal fibroblasts

“…Fortunately, emerging evidence indicates that the use of nano‐scale carrier can solve the above problems. For example, Dong reported that FBS‐derived exosomes as a nano‐scale carrier of icariin were more effective than icariin alone in the treatment of bone loss (Dong et al, 2021). Therefore, nano‐antioxidant therapy is to be expected in the future, whether in kidney diseases, toxicity‐related diseases, or other diseases.…”

Development of an Icariin-Loaded Bilosome-Melittin Formulation with Improved Anticancer Activity against Cancerous Pancreatic Cells

“…The first evidence of a relevant improvement in the anticancer activity of ICA-BM is clearly demonstrated in Figure 4, in which the IC 50 of this optimized formulation, a parameter often used to compare the antiproliferative activity and the toxic potential of different antineoplastic drugs [35], is equal to 2.79 ± 0.2 µM, a value ten times lower compared to that of ICA-Raw (22.3 ± 3.4). Most probably the observed enhanced cytotoxic effects observed when employing the optimized formula are coming from the ability of BM to enhance the poor solubility of ICA, ensuring a higher intracellular availability [12]; in fact, despite its promising anticancer activity, ICA is characterized by poor bioavailability due to low solubility and permeability [11]. The relevance of this result is also connected to the fact that cancer patients often encounter severe adverse effects attributable to the necessity of administering high doses of the drug [36], so the development of new formulations able to maximize the clinical efficacy, then reducing the doses, is of great importance.…”

“…Based on the above, ICA represents an effective asset against pancreatic cancer. Despite its promising anticancer activity, ICA suffers from the shortcomings of poor bioavailability due to poor solubility and permeability [11]. In this regard, nanocarriers can be of great help, improving the bioavailability of ICA by increasing the solubility and permeability across the biological membranes [12], which could enhance anticancer activity against pancreatic cancer.…”